Cancer is a disease state characterized by the uncontrolled proliferation of genetically altered tissue cells. There have been several chemotherapeutic approaches developed to target cancer. These include alkylating and anti-mitotic agents, anti-metabolites and anti-tumor antibiotics. Such therapeutic agents act preferentially on rapidly proliferating cells such as cancer cells.
The utility of most of the anti-tumor agents currently in clinical use is limited by their inherent toxicity on normal healthy cells. Moreover, these agents often exhibit a low therapeutic index which further limits their medical utility. Furthermore, in view of their low therapeutic index, such agents are frequently administered at dosages encroaching the patient tolerable limit in order to achieve any significant therapeutic effect.
Breast and Prostate Cancer
Steroidal hormones play an important role in the growth of androgen and estrogen sensitive cancers, both of which account for about 35% of all cancers on men and women in Canada [1-3]. Inhibiting the action of these steroids by blocking their respective receptors has led to the development of numerous candidate therapies. The implementation of some these therapies has led to promising results, particularly in the treatment of prostate cancer (use of an anti-androgen in combination with a LHRH agonist) and breast cancer (anti-estrogen) [4]. However, drug resistance is observed following prolonged periods of exposure to such therapies, such that an evolution toward hormone independence is observed [5]. In such cases, classical chemotherapy (e.g. Doxorubicin) with its numerous side-effects becomes the treatment of choice in order to halt the evolution of the disease [6].
Ovarian Cancer
Ovarian cancer affects more than 200,000 women around the world, making it the 7th most common type of cancer [7]. In North America alone, more than 25,000 women are diagnosed annually with ovarian cancer, of which about 65% will succumb to the disease [8]. Notwithstanding the considerable amount of progress achieved in the 80's with the advent of platinum-based chemotherapeutic agents (induce cross-linking of subunits of DNA), little positive impact was observed on the mortality rate [9]. The most frequently used chemotherapeutic agents, paclitaxel (mitotic inhibitor) and cisplatin, have shown an average survival rate ranging from 26 to 40 months [10]. However, these agents were also shown to exhibit considerable side effects which are mainly due to their inherent general toxicity [11].
Leukemia
Leukemia remains the most frequently encountered type of cancer in Canadian children ranging in age from 0 to 14 years, with a mortality rate of 36% [12]. Even though its impact is less on the population at large, it remains one of the cancers having the highest mortality rate. Depending on which kind of blood cell is affected, leukemia can be divided into lymphoblastic or lymphocytic leukemias and myeloid or myelogenous leukemias [13]. Notwithstanding the efficacy of some of the classical anticancer agents, most display a cytotoxicity that extends to normal healthy cells, in addition to being subject to the development of some form of chemoresistance following prolonged periods of exposure [14-16].
British Patent 1,398,050 issued to Tuba Z. et al. on Jun. 18, 1975 discloses 2β,16β-bis-piperazino-androstane derivatives and salts thereof having the general formulas I and II respectively:

wherein R represents hydrogen or a C1-7 acyl group; R1 represents a C1-6 alkyl group, acetoxyethyl group, allyl group, or hydroxyethyl group; R2 represents hydrogen, a C1-6 alkyl group, allyl group or benzyl group; X stands for hydrogen; Y represents hydroxy or a C1-7 acyloxy group; or X and Y together may form an oxo group; and Z represents a chloride, bromide, iodide, hydroxy, mesyloxy or tosyloxy anion. These compounds were disclosed as possessing neuromuscular blocking activity.
The present disclosure refers to a number of documents, the content of which is herein incorporated by reference in their entirety.